Details for Patent: 6,743,777

Title:	Cyclic peptide antifungal agents and process for preparation thereof
Abstract:	Provided are compounds of the formula (1): ##STR1## wherein R' is hydrogen, methyl or NH.sub.2 C(O)CH.sub.2 --; R" and R'" are independently methyl or hydrogen; R adn R.sup.y are independently hydroxy or hydrogen; R.sub.1 is hydroxy, hydrogen, or hydroxysulfonyloxy; R.sub.7 is hydroxy, hydrogen, hydroxysulfonyloxy or phosphonooxy; R.sub.2 is a novel acyl side chain. Also provided are novel formulations, methods of inhibiting fungal and parasitic activity, and a process for preparing dideoxy (R=H) forms of the compounds.
Inventor(s):	Burkhardt; Frederick J. (Indianapolis, IN), Debono; Manuel (Indianapolis, IN), Nissen; Jeffrey S. (Indianapolis, IN), Turner, Jr.; William W. (Bloomington, IN)
Assignee:	Eli Lilly and Company (Indianapolis, IN)
Filing Date:	Feb 27, 2002
Application Number:	10/087,088
Claims:	1. A pharmaceutical formulation comprising a compound having the following formula: ##STR255## and a pharmaceutically acceptable carrier. 2. A method for inhibiting parasitic activity comprising contacting a formulation of claim 1 with a parasite. 3. A method of inhibiting fungal activity comprising contacting a formulation of claim 1 with a fungus. 4. A method of inhibiting the growth of organisms responsible for opportunistic infections in immunosuppressed individuals comprising administering a formulation of claim 1 to said individual. 5. A method of inhibiting the growth of Pneumocystis carinii comprising contacting a formulation of claim 1 with Pneumocystis carinii. 6. A pharmaceutical formulation comprising a compound represented by the formula ##STR256## wherein R is --O(CH.sub.2).sub.3 CH.sub.3, --O(CH.sub.2).sub.4 CH.sub.3, --O(CH.sub.2).sub.5 CH.sub.3, --O(CH.sub.2).sub.2 O(CH.sub.2).sub.3 CH.sub.3, or --O(CH.sub.2).sub.2 OC(CH.sub.3).sub.3 and a pharmaceutically acceptable carrier. 7. The formulation of claim 6, wherein R is --O(CH.sub.2).sub.4 CH.sub.3. 8. A method for inhibiting parasitic activity comprising contacting a formulation of claim 6 with a parasite. 9. The method of claim 8, wherein R is --O(CH.sub.2).sub.4 CH.sub.3. 10. A method of inhibiting fungal activity comprising contacting a formulation of claim 6 with a fungus. 11. The method of claim 10, wherein R is --O(CH.sub.2).sub.4 CH.sub.3. 12. A method of inhibiting the growth of organisms responsible for opportunistic infections in immunosuppressed individuals comprising administering a formulation of claim 6 to said individual. 13. The method of claim 12, wherein R is --O(CH.sub.2).sub.4 CH.sub.3. 14. A method of inhibiting the growth of Pneumocystis carinii comprising contacting a formulation of claim 6 with Pneumocystis carinii. 15. The method of claim 14, wherein R is --O(CH.sub.2).sub.4 CH.sub.3. 16. A pharmaceutical formulation comprising a compound represented by the formula ##STR257## and a pharmaceutically acceptable carrier. 17. A pharmaceutical formulation comprising a pharmaceutically acceptable salt of the formulation according to claim 16. 18. A method for inhibiting parasitic activity comprising contacting a formulation of claim 16 with a parasite. 19. A method of inhibiting fungal activity comprising contacting a formulation of claim 16 with a fungus. 20. A method of inhibiting the growth of organisms responsible for opportunistic infections in immunosuppressed individuals comprising administering a formulation of claim 16 to said individual. 21. A method of inhibiting the growth of Pneumocystis carinii comprising contacting a formulation of claim 16 with Pneumocystis carinii.